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一种新型血管舒张剂,N-(6-氨基己基)-5-氯-1-萘磺酰胺,它作用于血管平滑肌肌动球蛋白。

A novel vascular relaxing agent, N-(6--aminohexyl)-5-chloro-1-naphthalensulfonamide which affects vascular smooth muscle actomyosin.

作者信息

Hidaka H, Asano M, Iwadare S, Matsumoto I, Totsuka T, Aoki N

出版信息

J Pharmacol Exp Ther. 1978 Oct;207(1):8-15.

PMID:702353
Abstract

The relaxing effect and possible mechanism of N-(6-aminohexyl)-5-chloro-1-naphthalenesulfonamide (W-7) on isolated rabbit artery were investigated. The addition of W-7 in concentrations ranging from 1 X 10(-6) to 3 X 10(-4) M caused a significant relaxation of isolated rabbit vascular strips contracted by KCl, prostaglandin F2alpha, norepinephrine, histamine, CaCl2, serotonin or angiotensin II. W-7 also caused a shift to the right of the dose-response curves for all agonists tested. Propranolol and atropine did not affect W-7 induced relaxation, suggesting that this drug does not act through beta adrenergic or cholinergic receptors. Superprecipitation of actomyosin from bovine aorta smooth muscle was inhibited by the addition of W-7 in a dose-dependent fashion. The concentration of W-7 which inhibited superprecipitation of bovine aorta smooth muscle actomyosin was in good agreement with the dose producing relaxation of isolated vascular strips. These facts suggest that W-7 produces relaxation of isolated vascular strips by inhibiting actin and myosin interaction.

摘要

研究了N-(6-氨基己基)-5-氯-1-萘磺酰胺(W-7)对离体兔动脉的舒张作用及其可能机制。加入浓度范围为1×10⁻⁶至3×10⁻⁴ M的W-7可使由氯化钾、前列腺素F2α、去甲肾上腺素、组胺、氯化钙、5-羟色胺或血管紧张素II收缩的离体兔血管条显著舒张。W-7还使所有受试激动剂的剂量-反应曲线右移。普萘洛尔和阿托品不影响W-7诱导的舒张,提示该药物并非通过β肾上腺素能或胆碱能受体起作用。加入W-7可剂量依赖性地抑制牛主动脉平滑肌中肌动球蛋白的超沉淀。抑制牛主动脉平滑肌肌动球蛋白超沉淀的W-7浓度与产生离体血管条舒张的剂量高度一致。这些事实提示,W-7通过抑制肌动蛋白和肌球蛋白的相互作用使离体血管条舒张。

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